Pharmacokinetics and Pharmacodynamics III Flashcards
(25 cards)
Name four drug classes with high efficacy.
Analgesic (pain) medications, antibiotics, antihistamines, decongestants (p.229)
How is efficacy altered in partial vs full agonists?
Partial agonists have less efficacy than full agonists (p.229)
What is potency?
The amount of drug needed for a given effect (p.229)
How does potency relate to receptor affinity?
High potency indicates high affinity for a receptor (p.229)
Name three drug classes with high potency.
Chemotherapeutic (cancer) drugs, antihypertensive (blood pressure) drugs, anti-lipid (cholesterol) drugs (p.229)
On a graph illustrating receptor binding, a competitive antagonist will shift the agonist curve in what direction?
Shift to the right (parallel curve) indicating that higher doses are needed to reach the same efficacious level; This indicates a decrease in potency with no change in efficacy (p.229)
Name an example of a competitive antagonist interaction.
Diazepam + flumazenil on GABA receptor (p.229)
On a graph illustrating receptor binding, a noncompetitive antagonist will shift the agonist curve in what direction?
Shifts curve down to indicate decreased efficacy which cannot be overcome by adding additional agonist substrate (p.229)
Name an example of a noncompetitive antagonist interaction.
NE + Phenoxybenzamine on a-receptors (p.229)
On a graph illustrating receptor binding, how does a partial agonist compare to an agonist?
Partial agonists act at the same site as full agonists, but with reduced maximal effect (i.e. decreased efficacy). Potency is a different variable and can be either increased or decreased (p.229)
Name an example of a partial agonist and its related full agonist.
Morphine is a full agonist; buprenorphine is a partial agonist at the opioid u receptor (p.229)
How do you calculate Therapeutic Index?
LD50/ED50 = median lethal dose/ median effective dose (p.229)
Name four examples of drugs with characteristically low therapeutic indexes.
Digoxin, lithium, theophylline, warfarin (p.229)
What is the therapeutic window?
A measure of clinical drug safety. Ranges from minimum effective dose to minimum toxic dose (p.229)
What tissue types may be controlled by parasympathetic and sympathetic stimulation?
Cardiac cells, smooth muscle cells, gland cells, nerve terminals (p.230)
What branch of the autonomic nervous system controls sweat glands?
Sympathetic (p.230)
What branch of the autonomic nervous system controls renal vasculature?
Sympathetic (p.230)
What branch of the nervous system controls skeletal muscle?
The somatic nervous system (p.230)
What branch of the autonomic nervous system controls the adrenal medulla?
Sympathetic (p.230)
What distinguishes sympathetic innervation of the adrenal medulla and sweat glands from all other sympathetic innervation?
Innervation by cholinergic fibers (ACh) (p.230)
What is the mechanism of action of botulinum toxin?
Prevents release of NTs at all cholinergic terminals (p.230)
Name the two types of ACh receptors.
Nicotinic and Muscarinic (p.230)
What types of receptors are Nicotinic ACh receptors?
Ligand-gated Na/K channels (p.230)
Where are Nicotinic neuronal receptors found (Nn)?
Autonomic ganglia (p.230)
